[11C]PE21: A highly selective radioligand for PET examination of the dopamine transporter in monkey and human brain

European Journal of Nuclear Medicine and Molecular Imaging

Volumn 30, Issue 9, 2003, Pages 1220-1230

  Halldin, Christer ^a   Erixon Lindroth, Nina ^a   Pauli, Stefan ^a   Chou, Yuan Hwa ^a   Okubo, Yoshiro ^a   Karlsson, Per ^a   Lundkvist, Camilla ^a   Olsson, Hans ^a   Guilloteau, Denis ^b   Emond, Patrick ^b   Farde, Lars ^a  

^a KAROLINSKA UNIVERSITY HOSPITAL   (Sweden)

^b UNIVERSITÉ DE TOURS   (France)

Author keywords

Brain; Dopamine transporter; PE2I; PET; Striatum; Substantia nigra

Indexed keywords

CITALOPRAM; COCAINE; DOPAMINE TRANSPORTER; MAPROTILINE; METHYL TRIFLATE C 11; N (3 IODOPROP 2 ENYL) 2BETA CARBOMETHOXY 3BETA (4 METHYLPHENYL)NORTROPANE C 11; RADIOLIGAND; RADIOPHARMACEUTICAL AGENT; UNCLASSIFIED DRUG; CARRIER PROTEIN; DIAGNOSTIC AGENT; MEMBRANE PROTEIN; N (3 IODOPROP 2 ENYL) 2 BETA CARBOMETHOXY 3 (4 METHYLPHENYL)NORTROPANE; N-(3-IODOPROP-2-ENYL)-2-BETA-CARBOMETHOXY-3-(4-METHYLPHENYL)NORTROPANE; NERVE PROTEIN; NORTROPANE DERIVATIVE; SLC6A3 PROTEIN, HUMAN;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BRAIN TISSUE; CEREBELLUM CORTEX; CONTROLLED STUDY; CORPUS STRIATUM; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN TISSUE; ISOTOPE LABELING; MONKEY; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; RADIOACTIVITY; SUBSTANTIA NIGRA; ADULT; ANIMAL; BLOOD; BRAIN; CASE REPORT; COMPARATIVE STUDY; COMPUTER ASSISTED EMISSION TOMOGRAPHY; EVALUATION; MACACA; MALE; METABOLIC CLEARANCE RATE; METABOLISM; METHODOLOGY; REPRODUCIBILITY; SCINTISCANNING; SENSITIVITY AND SPECIFICITY; TISSUE DISTRIBUTION; VALIDATION STUDY;

ADULT; ANIMALS; BRAIN; DOPAMINE PLASMA MEMBRANE TRANSPORT PROTEINS; HUMANS; MACACA FASCICULARIS; MALE; MEMBRANE GLYCOPROTEINS; MEMBRANE TRANSPORT PROTEINS; METABOLIC CLEARANCE RATE; NERVE TISSUE PROTEINS; NORTROPANES; RADIOPHARMACEUTICALS; REPRODUCIBILITY OF RESULTS; SENSITIVITY AND SPECIFICITY; TISSUE DISTRIBUTION; TOMOGRAPHY, EMISSION-COMPUTED;

EID: 0141447478     PISSN: 16197070     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00259-003-1212-3     Document Type: Article

References (48)

1. 123I]beta-CIT SPECT imaging of striatal dopamine transporter binding in Tourette's disorder. Am J Psychiatry 1995; 152:1359-1361.
2. 123I]beta-CIT SPECT. Am J Psychiatry 1998; 155:832-834.
3. 123I]β-CIT SPECT. J Neurol 1998; 245:14-20.
4. Laasonen-Balk T, Kuikka J, Viinamaki H, Husso-Saastamoinen M, Lehtonen J, Tiihonen J. Striatal dopamine transporter density in major depression. Psychopharmacology 1999; 144:282-285.
5. Dougherty DD, Bonab AA, Spencer TJ, Rauch SL, Madras BK, Fischman AJ. Dopamine transporter density in patients with attention deficit hyperactivity disorder. Lancet 1999; 354:2132-2133.
6. Krause KH, Dresel SH, Krause J, Kung HF, Tatsch K. Increased striatal dopamine transporter in adults patients with attention deficit hyperactivity disorder: effects of methylphenidate as measured by single photon emission computed tomography. Neurosci Lett 2000; 285:107-110.
7. 123I]beta-CIT SPECT imaging assessment of the rate of Parkinson's disease progression. Neurology 2001; 57:2089-2094.
8. Parkinson study group. Dopamine transporter brain imaging to assess the effects of pramipexole vs levedopa on Parkinson's disease progression. JAMA 2002; 287:1653-1667.
9. Halldin C, Gulyas B, Langer O, Farde L. Brain radioligands state of the art and new trends. Q J Nucl Med 2001; 45:139-152.
10. 123I]-2β-carbomethoxy-3β-(4-iodophenyl)tropane: High-affinity SPECT radiotracer of monoamine reuptake sites in brain. J Med Chem 1991; 34:3144-3146.
11. Innis RB, Seibyl JP, Scanley BE, Laruelle M, Abi-Dargham A, Wallace E, Baldwin RM, Zea-Ponce Y, Zoghbi S, Wang S, Gao Y, Neumeyer JL, Charney DS, Hoffer PB, Marek KL. Single photon computed tomographic imaging demonstrates loss of striatal dopamine transporters on Parkinson disease. Proc Natl Acad Sci USA 1993; 90:11965-11969.
12. 11C]β-CIT, a cocaine analogue preparation, autoradiography and preliminary PET investigations. Nucl Med Biol 1993; 20:249-255.
13. 11C]methyl triflate. Nucl Med Biol 1995; 22:235-239.
14. 11C]β-CIT binding to monoamine transporters in the monkey and human brain. Synapse 1994; 16:93-103.
15. Neumeyer JL, Wang S, Gao Y, Milius RA, Kula NS, Campbell A, Baldessarini RJ, Zea-Ponce Y, Baldwin RM, Innis RB. N-ω-Fluoroalkyl analogs of (1R)-2β-carbomethoxy-3β-(iodophenyl)tropane (β-CIT): radiotracers for positron emission tomography and single photon emission computed tomography imaging of dopamine transporters. J Med Chem 1994; 37:1558-1561.
16. 123I]N-ω-fluoroalkyl-2β -carboxy-3β-(4-iodophenyl)nortropane esters in baboons. Nucl Med Biol 1995; 22:211-219.
17. Kuikka JT, Bergström KA, Ahonen A, Hiltunen J, Haukka J, Länsimies E, Wang S, Neumeyer JL. Comparison of iodine-123 labeled 2β-carbomethoxy-3β-(4-iodophenyl)tropane (β-CIT) and 2β-carbomethoxy-3β-(4-iodophenyl)-N-(3-fluoropropyl)nortropane (β-CIT-FP) for the dopamine transporters in the living human brain. Eur J Nucl Med 1995; 22:682-686.
18. 11C]β-CIT-FP for quantitation of the dopamine transporter. Nucl Med Biol 1997; 24:621-627.
19. 18F]N-3-fluoropropyl-2-β-carbomethoxy-3-β-(4-iodophenyl) nortropane and the first human study with positron emission tomography. Nucl Med Biol 1996; 23:999-1004.
20. 11C]β-CIT-FE, a radioligand for quantitation of dopamine transporters in the living brain using positron emission tomography. Synapse 1996; 22:386-390.
21. 11C]β-CIT-FE, binding to the dopamine transporter in the monkey and human brain. Int J Neuropsychopharm 2000; 3:203-214.
22. 125C]β-OCIT for dopamine transporter visualisation: autoradiographic evaluation in the human brain. Nucl Med Biol 1997; 24:629-634.
23. 11C]WIN 35,428. Synapse 1993; 15:130-142.
24. 18F)WIN 35,428], a radioligand to study the dopamine transporter with PET: characterization in human subjects. Synapse 1998; 28:244-250.
25. Fischman AJ, Bonab AA, Babich JW, Palmer EP, Alpert NM, Elmaleh DR, Callahan RJ, Barrow SA, Graham W, Meltzer PC, Hanson RN, Madras BK. Rapid detection of Parkinson's disease by SPECT with altropane: a selective ligand for dopamine transporters. Synapse 1998; 29:128-141.
26. Chalon S, Garreau L, Emond P, Zimmer L, Vilar MP, Besnard J-C, Guilloteau D. Pharmacological characterization of (E)-N(3-iodoprop-2-enyl)-2β-carbomethoxy-3β-(4′-methylphenyl) nortropane as a selective and potent inhibitor of the neuronal dopamine transporter. J Pharmacol Exp 1999; 291:648-654.
27. 125I]PE2I. Neuroimage 1999; 9:108-116.
28. Emond P, Garreau L, Chalon S, Boazi M, Caillet M, Bricard J, Frangin Y, Mauclaire L, Besnard J-C, Guilloteau D. Synthesis and ligand binding of nortropane derivatives: N-substituted-2β-carbomethoxy-3β-(4′ -iodophenyl)nortropane and N-(3-iodoprop-2E-enyl)-2β-carbomethoxy-3β -(3′,4′-disubstituted phenyl)nortropane. New affinity and selectivity compounds for the dopamine transporter. J Med Chem 1997; 40:1366-1372.
29. Guilloteau D, Emond P, Baulieu JL, Garreau L, Frangin Y, Pourcelot L, Mauclaire L, Besnard J-C, Chalon S. Exploration of the dopamine transporter: in vitro and in vivo characterization of a high-affinity and high-specificity iodinated tropane derivative (E)-N-(3-iodoprop-2-enyl)-2β -carbomethoxy-3β-(4′-methylphenyl)nor-tropane (PE2I). Nucl Med Biol 1998; 25:331-337.
30. Kuikka JK, Baulieu JL, Hiltunen J, Halldin C, Bergström K, Farde L, Emond P, Chalon S, Yu M, Nikula T, Laitinen T, Karhu J, Tupala E, Hallikainen T, Kolehmainen V, Mauclaire L, Maziere B, Tiihonen J, Guilloteau D. Pharmacokinetics and dosimetry of iodine-123 labelled PE2I in humans, a radioligand for dopamine transporter imaging. Eur J Nucl Med 1998; 25:531-534.
31. 11C]methyl triflate. Appl Radiat Isot 1992; 43:1383-1385.
32. 11C]FLB457 by the use of GE Medical Systems PETtrace MeI Microlab. J Lab Compd Radiopharm 2000; 43:331-338.
33. Wienhard K, Dahlbom M, Eriksson L, Michel C, Bruckbauer T, Pietrzyk U, Heiss W-D. The ECAT EXACT HR: performance of a new high resolution positron scanner. J Comput Assist Tomogr 1994; 18:110-118.
34. 11C]NNC 756 as new radioligands for the D1-dopamine receptor. Psychopharmacology 1993; 113:149-156.
35. Andersen P. The dopamine uptake inhibitor GBR12909: selectivity and molecular mechanisms of action. Eur J Pharmacol 1989; 166:493-504.
36. Pinder R, Brogden R, Speight T, Avery G. Maprotiline: a review of its pharmacological properties and therapeutic efficacy in mental depressive states. Drugs 1977; 13:321-352.
37. Hyttel J. Citalopram: Pharmacological profile of a specific serotonin uptake inhibitor with antidepressant activity. Prog Neuropsychopharmacol Biol Psychiatry 1982; 6:277-295.
38. Bergström M, Boëthius J, Eriksson L, Greitz T, Ribbe T, Widén L. Head fixation device for reproducible position alignment in transmission CT and positron emission tomography. J Comput Assist Tomogr 1981; 5:136-141.
39. Eriksson L, Holte S, Bohm C, Kesselberg M, Hovander B. Automated blood sampling system for positron emission tomography. IEEE Trans Nucl Sci 1988; 35:703-707.
40. Halldin C, Swahn C-G, Farde L, Sedvall G. Radioligand disposition and metabolism. Key information in early drug development. In: Comar D, ed. PET for drug development and evaluation. Dordrecht: Kluwer Academic; 1995:55-65.
41. Madras BK, Gracz LM, Meltzer PC, Liang AY, Elmaleh DR, Kaufman MJ, Fischman AJ. Altropane, a SPECT or PET imaging probe for dopamine neurons. II. Distribution to dopamine-rich regions of primate brain. Synapse 1998; 29:105-115.
42. 11C]raclopride binding to D2-dopamine receptors studied by PET-a comparison to the saturation analysis. J Cerebr Blood Flow Metab 1989; 9:696-708.
43. 11C]raclopride binding. J Cereb Blood Flow Metab 1998; 18:941-950.
44. Drebin RA, Carpenter L, Hanrahan P. Volume rendering. Comput Graph 1988; 22:65-74.
45. Pauli S, Sedvall G. Three-dimensional visualization of the benzodiazepine receptor population within a living human brain using PET and MRI. Eur Arch Psychiatry Clin Neurosci 1997; 247:61-70.
46. 11C-raclopride. Psychopharmacology 1987; 92:278-284.
47. Halldin C, Farde L, Högberg T, Hall H, Ström P, Ohlberger A, Solin O. A comparative PET-study of five carbon-11 or fluorine-18 labelled salicylamides. Preparation and in vitro dopamine D-2 binding. Nucl Med Biol 1991; 18:871-881.
48. 11C-raclopride in living human brain-a search for extrastriatal central D2-dopamine receptors by PET. Psychopharmacology 1988; 94:471-478.